Results 41 to 50 of about 22,886 (216)

Characterization of HIV-1 integrase interaction with human Ku70 protein and initial implications for drug targeting

Scientific Reports, 2017
Human Ku70/Ku80 protein is known to influence HIV-1 replication. One of the possible reasons may be the protection of integrase from proteasomal degradation by Ku70 subunit. We demonstrated that recombinant HIV-1 integrase and Ku70 form a stable complex,
Andrey N. Anisenko, Ekaterina S. Knyazhanskaya, Artur O. Zalevsky, Julia Yu Agapkina, Aleksander I. Sizov, Timofey S. Zatsepin, Marina B. Gottikh   +6 more
doaj   +1 more source

Insights into the Dynamics and Binding Mechanisms of the Alkhumra Virus NS2B/NS3 Protease: A Molecular Dynamics Study

Advanced Theory and Simulations, EarlyView.
The ΔRMSF$\Delta {\rm RMSF}$ analysis reveals significant flexibility differences between free NS3 and the NS2B/NS3 complex, with notable deviations in specific regions. Key residues driving NS2B binding are identified, and the protonation state of catalytic serine affects oxyanion hole formation.
Jurica Novak, Shivananda Kandagalla, Ramesh Sistla   +2 more
wiley   +1 more source

Pre-Treatment Integrase Inhibitor Resistance and Natural Polymorphisms among HIV-1 Subtype C Infected Patients in Ethiopia

Viruses, 2022
Dolutegravir-based antiretroviral therapy (ART) has been scaled up in many developing countries, including Ethiopia. However, subtype-dependent polymorphic differences might influence the occurrence of HIV-drug-resistance mutations (HIVDRMs). We analyzed
Dawit Assefa Arimide, Zsófia Ilona Szojka, Kidist Zealiyas, Atsbeha Gebreegziabxier, Fekadu Adugna, Sviataslau Sasinovich, Per Björkman, Patrik Medstrand   +7 more
doaj   +1 more source

Approaches to repurposing reverse transcriptase antivirals in cancer

British Journal of Clinical Pharmacology, EarlyView.
This review highlights the role of reverse transcriptase (RT) inhibition in cellular regulation associated with non‐terminal repeat retrotransposons and endogenous retroviruses. Based on their pleiotropic characteristics, RT inhibitors (RTIs) are discussed as potential anticancer agents.
Richard Head, Saiful Islam, Jennifer H. Martin   +2 more
wiley   +1 more source

INSTIs and NNRTIs Potently Inhibit HIV-1 Polypurine Tract Mutants in a Single Round Infection Assay

Viruses, 2021
Integrase strand transfer inhibitors (INSTIs) are a class of antiretroviral compounds that prevent the insertion of a DNA copy of the viral genome into the host genome by targeting the viral enzyme integrase (IN).
Steven J. Smith, Andrea Ferris, Xuezhi Zhao, Gary Pauly, Joel P. Schneider, Terrence R. Burke, Stephen H. Hughes   +6 more
doaj   +1 more source

Factors Influencing the Binding of HIV‐1 Protease Inhibitors: Insights from Machine Learning Models

ChemMedChem, Accepted Article.
HIV‐1 protease inhibitors are crucial for antiviral therapies targeting acquired immunodeficiency syndrome (AIDS). Hundreds of HIV‐1 protease complexes with various ligands have been resolved and deposited in the Protein Data Bank. However, binding affinity measurements for these ligands are not always available.
Yaffa Shalit, Inbal Tuvi-Arad
wiley   +1 more source

The Drug-Induced Interface That Drives HIV-1 Integrase Hypermultimerization and Loss of Function

mBio, 2023
Allosteric HIV-1 integrase (IN) inhibitors (ALLINIs) are an emerging class of small molecules that disrupt viral maturation by inducing the aberrant multimerization of IN. Here, we present cocrystal structures of HIV-1 IN with two potent ALLINIs, namely,
Matthew R. Singer, Tung Dinh, Lev Levintov, Arun S. Annamalai, Juan S. Rey, Lorenzo Briganti, Nicola J. Cook, Valerie E. Pye, Ian A. Taylor, Kyungjin Kim, Alan N. Engelman, Baek Kim, Juan R. Perilla, Mamuka Kvaratskhelia, Peter Cherepanov   +14 more
doaj   +1 more source

A Randomized Phase 1 Study Evaluating Pharmacokinetics, Safety, and Tolerability of a High‐Concentration, Long‐Acting Cabotegravir Formulation in Adults Without HIV

Clinical Pharmacology in Drug Development, EarlyView.
Abstract Long‐acting (LA) cabotegravir 200‐mg/mL (CAB200) injections are approved for HIV‐1 prevention and as a complete LA HIV‐1 treatment regimen with rilpivirine. A high‐concentration suspension formulation, cabotegravir 400 mg/mL (CAB400‐D), was developed to enable less frequent dosing and self‐administration. This phase 1, double‐blind, randomized
Kelong Han, Paul Benn, Jörg Sievers, David Dorey, Michael Warwick‐Sanders, Randa Hareedy, Louise Harkness, Claudia Leemereise, Kjersten Offenbecker, Christina Donatti, Darin B. Brimhall, Christian Schwabe, Craig Boyle, Michael A. Hassman, Steve Knowles, Ronald D'Amico, William R. Spreen   +16 more
wiley   +1 more source

Nature Inspired Delivery Vehicles for CRISPR‐Based Genome Editing

Small, EarlyView.
The review highlights nature‐inspired nanocarriers for CRISPR delivery, emphasizing viral vectors, extracellular vesicles, liposomes, and lipid nanoparticles. It discusses their roles in improving specificity, minimizing immunogenicity, and overcoming barriers in genome editing. Recent advancements, challenges, and therapeutic applications are explored,
Elizabeth Maria Clarissa, Mamata Karmacharya, Hyunmin Choi, Sumit Kumar, Yoon‐Kyoung Cho   +4 more
wiley   +1 more source

PIAS3 modulate HIV-1 integrase SUMOylation [PDF]

Retrovirology, 2011
Background HIV-1 hijacks cellular machineries to replicate. Posttranslational modifications, like acetylation, phosphorylation or ubiquitination are not exception. We are interested in studying the interplay between HIV-1 and the SUMOylation pathway. SUMOylation consists in the covalent attachment of SUMO (Small Ubiquitin-like Modifier) proteins to a ...
Beauclair, Guillaume, Paris, Joris, Magne, Fabien, Zamborlini, Alessia, Saϊb, Ali   +4 more
openaire   +4 more sources